R-泊马度胺杂质 | 202271-90-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 中文名称: R-泊马度胺杂质
• 英文名称: (R)-(+)-4-amino-2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3-dione
• 英文别名: R(-)-4-amino-2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3-dione；(R)-pomalidomide；pomalidomide；(R)-(+)-4-aminothalidomide；R(-)-4-amino-thalidomide；R(-)-pomalidomide；Pomalidomide, (R)-；4-amino-2-[(3R)-2,6-dioxopiperidin-3-yl]isoindole-1,3-dione
• CAS: 202271-90-7
• 化学式: C₁₃H₁₁N₃O₄
• 分子量: 273.248
• InChiKey: UVSMNLNDYGZFPF-MRVPVSSYSA-N

物化性质

• 沸点：
  582.9±45.0 °C(Predicted)
• 密度：
  1.570±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-硝基-N-碳乙氧基邻苯二甲酰亚胺 在 palladium on activated charcoal 吡啶 、 盐酸 、 氯化亚砜 、 氢气 、 三乙胺 作用下， 以 二氯甲烷 、 丙酮 为溶剂， 生成 R-泊马度胺杂质
  参考文献：
  名称：

  Amino-substituted thalidomide analogs: Potent inhibitors of TNF-α production

  摘要：

  Thalidomide, (1), is a known inhibitor of TNF-alpha release in LPS stimulated human PBMC. Herein we describe the TNF-alpha inhibitory activity of amino substituted analogs of thalidomide (1) and its isoindolin-1-one analog, EM-12 (2). The 4-amino substituted analogs were found to be potent inhibitors of TNF-alpha release in LPS stimulated human PBMC. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00250-4

文献信息

• Processes for the preparation of 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds
  申请人：Ge Chuanshen

  公开号：US20070004920A1

  公开（公告）日：2007-01-04

  The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are usefuil, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-α. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.

  本发明提供了新的制备未取代和取代的4-氨基-2-(2,6-二氧杂哌啶-3-基)异吲哚啉-1,3-二酮化合物的方法，这些化合物例如可用于预防或治疗与TNF-α水平或活性异常升高相关的疾病或状况。本发明能够提供改进和/或有效的商业生产未取代和取代的4-氨基-2-(2,6-二氧杂哌啶-3-基)异吲哚啉-1,3-二酮化合物的方法，包括但不限于未取代的4-氨基-2-(2,6-二氧杂哌啶-3-基)异吲哚啉-1,3-二酮。
• Substituted 2(2,6-dioxopiperidin-3-yl)isoindolines
  申请人：Celgene Corporation

  公开号：US06335349B1

  公开（公告）日：2002-01-01

  Substituted 1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)isoindolines and 1-oxo-2-(2,6-dioxo-piperidin-3-yl)isoindolines reduce the levels of TNF&agr; in a mammal and are useful in treating oncogenic conditions, inflammation, and autoimmune diseases. Typical embodiments are 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafluoroiso-indoline and 1,3-dioxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4-aminoisoindoline.

  1,3-二氧代-2-(2,6-二氧代哌啶-3-基)异吲哚烷酮和1-氧代-2-(2,6-二氧代哌啶-3-基)异吲哚烷酮可降低哺乳动物体内TNF&agr;的水平，并可用于治疗肿瘤性疾病、炎症和自身免疫疾病。典型实施例包括1-氧代-2-(2,6-二氧代-3-甲基哌啶-3-基)-4,5,6,7-四氟异吲哚烷酮和1,3-二氧代-2-(2,6-二氧代-3-甲基哌啶-3-基)-4-氨基异吲哚烷酮。
• HETEROARYL COMPOUNDS AND USES THEREOF
  申请人：Celgene Avilomics Research, Inc.

  公开号：US20150174128A1

  公开（公告）日：2015-06-25

  The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

  本发明提供了化合物、药学上可接受的组合物以及使用它们的方法。
• [EN] METHODS FOR THE TREATMENT OF LOCALLY ADVANCED BREAST CANCER<br/>[FR] MÉTHODES POUR LE TRAITEMENT DU CANCER DU SEIN LOCALEMENT AVANCÉ
  申请人：CELGENE CORP

  公开号：WO2014039960A1

  公开（公告）日：2014-03-13

  Provided herein are methods of treating, preventing and/or managing locally advanced breast cancer, including inflammatory breast cancer, which comprise administering to a patient one or more immunomodulatory compounds or enantiomers or mixtures of enantiomers thereof, or pharmaceutically acceptable salts, solvates, hydrates, co-crystals, clathrates, or polymorphs thereof.

  本文提供了治疗、预防和/或管理局部晚期乳腺癌的方法，包括炎性乳腺癌，该方法包括向患者施用一种或多种免疫调节化合物或其对映体或对映体混合物，或其药用可接受的盐、溶剂化合物、水合物、共晶体、包合物或多形体。
• Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor
  申请人：Lopez-Girona Antonia

  公开号：US09365640B2

  公开（公告）日：2016-06-14

  Uses of the protein cereblon as a predictor of clinical sensitivity to cancer, inflammatory diseases, and patient response to drug treatment.

  将蛋白质 cereblon 用作癌症、炎症性疾病的临床敏感性预测以及患者对药物治疗的反应的预测。